金龙胆草化学成分及其抗溃疡活性研究(Ⅰ)

Chemical constituents and their antiulcerogenic studies on whole herb of Conyza blinii (Ⅰ)

目的研究金龙胆草Conyza blinii的化学成分及其抗溃疡活性。方法采用溶剂提取、重结晶和硅胶、聚酰胺柱色谱方法分离纯化，根据氢谱、碳谱、质谱以及与对照品共薄层色谱鉴定化合物的结构。用幽门结扎大鼠模型进行抗溃疡活性筛选。结果从金龙胆草的乙醇提取物中分离鉴定了8个化合物：5，8，3’，4’-四羟基-7-甲氧基黄酮（Ⅰ）、5，8，4’-三羟基-7，3＇-二甲氧基黄酮（Ⅰ）、β-谷甾醇（Ⅲ）、菠甾醇（Ⅳ）、正二十六烷酸（Ⅴ）、5，7-二羟基-3，3’，4＇-三甲氧基黄酮（Ⅵ）、5，7-二羟基-3，8，4’-三甲氧基黄酮（Ⅵ）和苦蒿素（Ⅶ）。苦蒿素能明显减少模型大鼠胃溃疡面积，明显减少胃黏膜组织中的MDA的水平。结论化合物Ⅰ～Ⅲ和Ⅴ～Ⅵ为首次从该植物中分离得到。苦蒿素对幽门结扎大鼠胃溃疡的形成有明显抑制作用，其可能作用机制与抑制胃黏膜组织中MDA的生成有关。

Objective To study the chemical constituents in the whole herb of Conyza blinii and seek its antiulcerogenic principles. Methods Compounds were separated and purified by solvent extraction, recrystallization, and chromatography on silica gel and polyamide column. Their structures were elucidated on the basis of ^1H-NMR, ^13C-NMR, and MS spectral data and co-TLC with authentic samples. Pylorusligated rat model was used for the evaluation of antiulcerogenic activity. Results Eight compounds were identified： 5, 8, 3＇, 4＇-tetrahydroxy-7-methoxy flavone （Ⅰ）, 5, 8, 4＇-trihydroxy-7, 3＇-dimethoxy flavone （Ⅱ）, β-sitosterol （Ⅲ）, spinasterol （Ⅳ）.n-hexacosanic acid （Ⅴ）, 5, 7-dihydroxy-3, 3＇, 4＇- trimethoxy flavone （Ⅵ）, 5, 7-dihydroxy-3, 8, 4＇-trimethoxy flavone （Ⅶ）, blinin （Ⅷ）. Blinin could significantly narrow the ulcer area and lower the level of gastric mucous MDA. Conclusion Compounds Ⅰ -- Ⅲ and Ⅴ --Ⅷ are obtained from the title plant for the first time. Blinin is found to possess significant antiulcer property.